Lysophosphatidic acid-1-receptor targeting agents for fibrosis.

Abstract : INTRODUCTION: The presence of fibrosis is associated with alterations in organ architecture and is responsible for the morbidity of diseases including pneumopathies, systemic sclerosis, liver cirrhosis, chronic cardiovascular diseases, progressive kidney diseases and diabetes. Although a growing number of pro-fibrotic molecules, mediators and other pathways have been reported, there are currently very few antifibrotic molecules being evaluated in clinical trials. AREAS COVERED: Current knowledge about the contribution of lysophosphatidic acid (LPA), a bioactive mediator acting via specific G-protein coupled receptors (LPAR), in the etiology of fibrosis. In a number of organs, fibrosis is associated with increased LPA production as well as with increased expression of some LPAR subtypes (mainly LPA1R). LPAR(-/-) knockout mice and treatment of animal models with specific antagonists clearly demonstrate the contribution of LPA1R subtype to the development of kidney, lung, vascular and dermal fibrosis. The involvement of LPA in liver fibrosis is also strongly suspected but still unproven. EXPERT OPINION: Experiments in animal models clearly demonstrate that LPA1R antagonists have interesting anti-fibrotic potencies. This reveals promising perspectives for the design of new therapeutic approaches to prevent fibrosis-associated diseases. Nevertheless, the number of efficient LPA1R antagonists currently available is still low, and none of them has been used in clinical trials so far.
Type de document :
Article dans une revue
Expert Opinion on Investigational Drugs, Taylor & Francis, 2011, 20 (5), pp.657-67. 〈10.1517/13543784.2011.566864〉
Liste complète des métadonnées

http://www.hal.inserm.fr/inserm-00617587
Contributeur : Marie Francoise Simon <>
Soumis le : lundi 29 août 2011 - 16:45:31
Dernière modification le : jeudi 4 octobre 2018 - 09:50:09

Identifiants

Collections

Citation

Chloé Rancoule, Jean-Philippe Pradère, Julien Gonzalez, Julie Klein, Philippe Valet, et al.. Lysophosphatidic acid-1-receptor targeting agents for fibrosis.. Expert Opinion on Investigational Drugs, Taylor & Francis, 2011, 20 (5), pp.657-67. 〈10.1517/13543784.2011.566864〉. 〈inserm-00617587〉

Partager

Métriques

Consultations de la notice

105